Lerupa

Uses

Lerupa is used for the symptomatic treatment of seasonal & perennial allergic rhinitis and urticaria.

Lerupa is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Pruritus, Urticaria

How Lerupa works

Lerupa is a dual histamine H1 receptor and platelet activating (PAF) receptor antagonist . During allergic response mast cells undergo degranulation, releasing histamine and other substances . Histamine acts on H1 receptors to produce symptoms of nasal blockage, rhinorhea, itching, and swelling. PAF is produced from phospholipids cleaved by phospholipase A2. It acts to produce vascular leakage which contributes to rhinorhea and nasal blockage. By blocking both the H1 receptor and PAF receptor, rupatidine prevents these mediators from exerting their effects and so reduces the severity of allergic symptoms.

Dosage

Lerupa dosage

Lerupa Tablet: The recommended dosage is 10 mg once daily, with or without food.

Lerupa Oral Solution (Children aged 2 to 11 year):

• Children weighing 25 kg or more: 1 teaspoonful (5 ml) of oral solution once daily with or without food.
• Children weighing equal or more than 10 kg to less than 25 kg: 1/2 teaspoonful (2.5 ml) oral solution once daily with or without food.

Side Effects

The most common undesirable effects occurs somnolence, headache and fatigue. Other common undesirable effects include dizziness, asthenia and increase appetite.

Precaution

Administration of a dose of 10 mg daily of Lerupa has not shown significant effects on the function of the central nervous system as seen in specific studies done for psychomotor function. Nevetheless, the patient should take precaution in driving or managing machines. The administration of rupatadine with grape fruit juice is not recommended.

Interaction

CYP3A4 inhibitors like Erythromycin & Ketoconazole inhibits both the presystemic and systemic metabolism of Lerupa. Due to this potential interaction, it is not recommended to use Lerupa in combination with Ketoconazole, macrolides or any other inhibitors of CYP3A4. Co administration of Lerupa and CNS depressants or alcohol may increase CNS depressant effect.

Food Interaction

• Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of rupatadine.
• Take with or without food.

Volume of Distribution

The apparent volume of distribution is 9799 L .

Elimination Route

Rupatidine is rapidly absorbed with a Tmax of 1 h . Administration with a high fat meal increases exposure by 23% and increases Tmax to 2 h.

Half Life

The half life of elimination is 15.9 h in children 2-5 years old, 12.3 h in children 6-11 years old, 5.9 h in adults, and 8.7 h in geriatric patients .

Clearance

Systemic clearance is 1556.2 L/h in young adults and 798.2 L/h in geriatric patients .

Pregnancy & Breastfeeding use

Pregnancy category B2 (by TGA, Australia). There is no clinical data available on the exposure of Lerupa during pregnancy. Pregnant women should therefore not use Lerupa, unless the potential benefit outweighs the potential risk for the fetus. No information is available, whether Lerupa is excreted in the mother's milk. Therefore, it should not be used during lactation, unless the potential benefits for the mother justify the potential risk to the infant.

Contraindication

Hypersensitivity to Lerupa or to any of the excipients.

Special Warning

Elderly: Lerupa should be used with caution in elderly. No information is available that indicates the requirement of any dose adjustment in this population.

Children: Neither the safety nor the efficacy of Lerupa has been established in patients less than 12 years of age.

Patients with renal or hepatic insufficiency: Use of Lerupa is not recommended in patients with renal or hepatic insufficiency. As no relevant clinical data is available.

Innovators Monograph

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